摘要
[目的]设计合成具有较强驱蚊活性的化合物。[方法]以10-十一烯酰氯和3-(甲氨基)丙酸乙酯为起始原料,经1步反应成功制备10-十一烯酰氨基甲基丙酸乙酯,并经核磁及质谱表征验证其结构。参照GB 15193.3—2014方法进行毒性试验及按照GB/T 13917.9—2009方法进行室内和现场驱蚊试验。[结果]所述合成路线反应收率较高,10-十一烯酰氨基甲基丙酸乙酯的小鼠经口LD50>2000 mg/kg体质量,属于低毒。对白纹伊蚊(Aedes albopictus)的有效保护时间(h)随着浓度(%)增加而延长,在质量分数为10%浓度下,其室内有效保护时间为(8.3±1.0)h。对照药驱蚊酯(IR3535)和避蚊胺(DEET)的有效保护时间分别为(6.0±0.8)、(5.8±1.0)h。10-十一烯酰氨基甲基丙酸乙酯现场有效保护时间为7~8 h(7、8 h的保护率分别为100.00%、92.13%)。对照药驱蚊酯和避蚊胺的有效保护时间分别为5~6 h(5、6 h的保护率分别为100.00%、90.11%)和5~6 h(5、6 h的保护率分别为100.00%、89.01%)。[结论]10-十一烯酰氨基甲基丙酸乙酯性质稳定,驱蚊效果好,使用安全,具有良好的应用前景。
[Aims]This study aims to design and synthesize a compound with strong mosquito repellent activity.[Methods]Starting from10-undecenoyl chloride and ethyl 3-(methylamino)propionate,ethyl 10-undecenoylmethylamino propionate was prepared by one-step reaction.The structure was characterized by NMR and MS.The toxicity was assayed according to GB 15193.3-2014 and mosquito repellent was examined according to GB/T 13917.9-2009 in lab or in the field.[Results]The synthetic route had high reaction yield.The oral LD50 of ethyl 10-undecenoyl methylamino propionate in mice is more than 2000 mg/kg body weight,which means it belongs to low toxicity.The effective protection time against A.albopictus was prolonged with the increase of concentration(%).At the concentration of 10%,the indoor effective protection time was(8.3±1.0)h.The effective protection time of ethyl 3-(N-butylacetamido)propanoate(IR3535)and diethyltoluamide(DEET)were(6.0±0.8)and(5.8±1.0)h.The effective protection time of ethyl 10-undecenoyl methylamino propionate in the field was 7-8 h(the protection rates at 7 and 8 h were 100.00 and 92.13%).The effective protection time of IR3535 and DEET were 5-6 h(the protection rates at 5 and 6 h were 100.00 and 90.11%)and 5-6 h(the protection rates at 5 and 6 h were 100.00 and 89.01%).[Conclusions]Ethyl 10-undecenoyl methylamino propionate was a stable compound as an efficient and safe mosquito repellent with application prospect.
作者
吴华
戴建青
陈大嵩
黄鸿
郑基焕
WU Hua;DAI Jian-qing;CHEN Da-song;HUANG Hong;ZHENG Ji-huan(Guangdong Key Laboratory of Animal Conservation and Resource Utilization,Guangdong Public Laboratory ofWild Animal Conservation and Utilization,Guangdong Engineering Research Center for Mineral Oil Pesticides,Institute of Zoology,Guangdong Academy of Sciences,Guangzhou 510260,Guangdong,China)
出处
《农药》
CAS
CSCD
北大核心
2021年第11期786-789,共4页
Agrochemicals
基金
广州市科技计划项目(201804010020,201707010471,201607010084)。
